- HOME
- New Product and Technology
- Kurtoxin
Kurtoxin
The First Peptidic T-type Ca2+-Channel Blocker
Voltage-dependent Ca2+-channels are classified according to the nature of their α1 subunits. High voltage-activated channels (HVA) are composed of α1A-α1F/α1S, leading to L-, N-, P/Q- and R-type channels. Peptidic blockers specific for each channel are commercially available List of Ion Channel Blockers. Low voltage-activated channels (LVA) are encoded by α1G-α1I, which correspond to T-type channels. Although these channels are known to be blocked by Ni2+ ions, until recently there was no peptidic blocker for this particular channel.
Kurtoxin:
Lys-Ile-Asp-Gly-Tyr-Pro-Val-Asp-Tyr-Trp-Asn-Cys-Lys-Arg-Ile-Cys-Trp-Tyr-Asn-Asn- Lys-Tyr-Cys-Asn-Asp-Leu-Cys-Lys-Gly-Leu-Lys-Ala-Asp-Ser-Gly-Tyr-Cys-Trp-Gly-Trp- Thr-Leu-Ser-Cys-Tyr-Cys-Gln-Gly-Leu-Pro-Asp-Asn-Ala-Arg-Ile-Lys-Arg-Ser-Gly-Arg- Cys-Arg-Ala
However, in 1998, a new T-type channel blocker, kurtoxin, was isolated from the venom of the South African scorpion (Parabuthus transvaalicus). This compound is a 63 amino acid residue peptide with 4 intramolecular disulfide linkages[Nat. Neurosci., 1, 668 (1998) ]. Using the expressed α1G channel, the binding of kurtoxin was found to involve 1:1 stoichiometry with a Kd value of 15 nM. Almost complete inhibition by kurtoxin was observed for the α1G channel at 350 nM, whereas the α1H channel was blocked approximately 85% at the same concentration. α1A– α1C and α1E Channels were not affected at 350 nM, indicating the specific blocking activity of kurtoxin for the expressed T-type channels. Because of the sequence similarity with α-scorpion toxins, kurtoxin binds to voltage-gated Na+ channels and slows their inactivation. Later, it was clarified that this peptide interacts with both HVA and LVA channels in rat central and peripheral neurons: i) N- and L-type channel currents were partially inhibited by 250-500 nM peptide (Kd=456 nM and 72 nM, respectively), ii) P-type Ba2+ current in Purkinje neurons was facilitated by 500 nM peptide (Kd=14 nM), and iii) Kd for thalamic T-type channels was 49 nM[J. Neurosci., 22, 2023 (2002) ]. The reason for this discrepancy between two reports remains to be clarified, however. T-type channel blocking activity of kurtoxin is attractive because this peptide does interact with both expressed and native T-type channels.
Kurtoxin is a useful blocker for T-type channels, especially when used in combination with the various blockers for HVA channels for further research investigations.
Code | Compound | Package |
4375-s | Kurtoxin | 0.1 mg vial |
Related Products
Code | Compound | Selectivity | Package |
4255-s | Calciseptine | L-type Blocker | 0.1 mg vial |
4310-s | Calcicludine | L-type Blocker | 0.1 mg vial |
4161-v | ω-Conotoxin GVIA | N-type Blocker | 0.5 mg vial |
4289-v | ω-Conotoxin MVIIA | N-type Blocker | 0.5 mg vial |
4284-v | ω-Conotoxin SVIB | N-type Blocker | 0.5 mg vial |
4256-s | ω-Agatoxin IVA | P-type Blocker | 0.1 mg vial |
4294-s | ω-Agatoxin TK | P-type Blocker | 0.1 mg vial |
4283-s | ω-Conotoxin MVIIC | P/Q-type Blocker | 0.1 mg vial |
4363-s | SNX-482 | R-type Blocker | 0.1 mg vial |